National Research Center of Engineering Technology For Utilization of Functional Ingredients From Botanicals, College of Horticulture and Landscape Architecture, Hunan Agricultural University, Changsha 410128, Hunan, China

Abstract Based on an established common pharmacophore of HIV-1 non-nucleoside reverse transcriptase inhibitors NNTTIs, a series of quinolin-2-one derivatives were synthesized and assayed for their in vitro activities against HIV-1 reverse transcriptase RT for the first time. Some of the tested compounds were active against HIV-1 RT. Compounds 4a2 and 4d2 showed inhibitory activities with IC50 values of 0.21 and 0.15 mM, respectively, with a mode of interaction with RT residues of the allosteric pocket similar to that of efavirenz.